A Two-step Drug Delivery System Based on Click Chemistry

Abstract

Researchers at the University of California, Davis have developed a technology that introduces a TCTS (Two-component Two-step) drug delivery system designed to enhance cancer treatment efficacy while minimizing toxicity.

Full Description

This invention presents a novel TCTS drug delivery strategy utilizing transformable nanoparticles and bioorthogonal click chemistry for targeted cancer therapy. It diverges from the conventional TCTS model employing antibody and protein nanoparticles by utilizing the combination of fibrillar transformable nanoplatform and small molecule drug conjugate.

In the traditional TCTS method, monoclonal antibodies (MAb) typically serve as the initial component for pre-targeting. In contrast, this innovative approach employs recently introduced transformable nanoparticles (TNP), which can self-assemble into micellar nanoparticles in aqueous condition, but transform into a nanofibrillar network with prolonged retention within the tumor microenvironment as the primary pre-targeting agent. The methyltetrazine-drug conjugate is then administered intravenously, which undergoes an in situ click reaction with the nanofibrillar network at the tumor sites. This approach promises enhanced therapeutic effectiveness and reduced side effects, offering a significant advancement in the treatment of cancers such as ovarian cancer.

Applications

• Targeted chemotherapy for ovarian and other solid tumors. 
• Delivery of immunomodulatory agents for cancer immunotherapy. 
• Advanced drug delivery platforms for personalized medicine. 
• Non-toxic nanoimmunotherapeutics for syngeneic breast cancer models. 
• Enhanced photothermal and photodynamic therapy via targeted nanoplatforms.

Features/Benefits

• Enhances targeting and retention in tumor microenvironment. 
• Reduces toxicity in normal tissues. 
• On-demand delivery of therapeutic payloads. 
• Applicable for a variety of therapeutic agents including chemotherapeutics and immunomodulators. 
• Highly specific bioorthogonal click chemistry for precise drug release. 
• Addresses the need for more efficacious and less toxic therapies against advanced cancers

Patent Status

Patent Pending